Cyclophosphamide must be activated by which organ before it can cause crosslinks between DNA strands?

Question

Cyclophosphamide must be activated by which organ before it can cause crosslinks between DNA strands?

BlackTom AI · Accepted Answer

The question asks which organ activates cyclophosphamide before it can cause crosslinks between DNA strands.
Option a) Heart: The heart is not the primary site of cyclophosphamide activation; it doesn’t perform the metabolic conversion to the active cytotoxic species.
Option b) Kidney: Although some drugs are excreted or activated in the kidney, activation of cyclophosphamide is not mainly occurring there.
Option c) Liver: Correct. Cyclophosphamide is a prodrug that requires activation by hepatic cytochrome P450 enzymes. In the liver, it is oxidized to 4-hydroxycyclophosphamide, which equilibrates to aldophosphamide and ultimately yields phosphoramide mustard, the species responsible for crosslinking DNA strands and exerting cytotoxic effects.
Option d) Brain: The brain is not the site of cyclophosphamide activation; it does not perform the metabolic oxidation steps required for activation.
Option e) Spleen: While the spleen has metabolic activity, the established primary organ for activating cyclophosphamide is the liver, not the spleen.
In summary, activation occurs in the liver via hepatic cytochrome P450 enzymes, enabling the formation of DNA crosslinking agents, whereas the other listed organs are not the sites of this critical metabolic activation.

Cyclophosphamide must be activated by which organ before it can cause crosslinks between DNA strands?

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